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br Conclusions GPCRs are versatile signaling
2021-09-13
Conclusions GPCRs are versatile signaling molecules regulating almost all physiological processes, including energy homeostasis and glucose homeostasis.105, 106 They also prove to be important therapeutic targets. Drugs targeting GPCRs account for 30% of current pharmaceutical sales. GPR40 is a m
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BDNF is intricately implicated in energy homeostasis Hamdouc
2021-09-13
BDNF is intricately implicated in energy homeostasis (Hamdouchi et al., 2016; Schwartz and Mobbs, 2012), regulation of mood (Sartorius et al., 2015) and adult neurogenesis (Taliaz et al., 2010; Waterhouse et al., 2012), our primary focus was to evaluate the effects of GPR40 stimulation on BDNF expre
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br FREE FATTY ACID RECEPTOR GPR br
2021-09-13
FREE FATTY ACID RECEPTOR 1 (GPR40) G-PROTEIN-COUPLED RECEPTOR 120 CONCLUSION Free fatty NVP-BEP800 receptors whose natural ligands are identified as FFAs having various lengths have been reported. They act as novel nutrient sensing receptors independent of PPARs and FABPs, and they are know
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Furthermore rs is the one which is studied
2021-09-13
Furthermore, rs17171119 is the one which is studied well so far. One of the earlier studies has reported the clinical outcome and impact of EZH2 SNPs (rs41277434, rs3757441, rs2302427 rs9177211 T> C) (Crea et al., 2012). The only coding SNP ID rs2302427 has been studied in various diseases such as h
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br Acknowledgements This research was supported by the Natur
2021-09-11
Acknowledgements This research was supported by the Natural Sciences and Engineering Council of Canada (NSERC) Discovery Grant awarded to RGM. LMW was supported in part by fellowships from the University of Regina and the Government of Saskatchewan Fish and Wildlife Development Fund (FWDF). We wo
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br STAR Methods br Acknowledgments This work was supported b
2021-09-11
STAR★Methods Acknowledgments This work was supported by the American Diabetes Association (grant 1-12-BS-161 to J.D.P.), an NIH predoctoral T32 in Autoimmunity and Immunopathology grant (AI089443-05 to D.M.P.), the NIH (grant DK099550 to H.M.T.), the American Association for Cancer Research (S
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As preclinical toxicity and efficacy both appear
2021-09-11
As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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The need for an inflammatory risk profile was recently
2021-09-11
The need for an ‘inflammatory risk profile’ was recently discussed by several investigators. The present study is all the more significant in that it shows that a phenomenon that is influenced by various atherosclerotic risk factors and acute phase proteins is, indeed, associated with a less favorab
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The nuclear repressor BACH is known to control HO expression
2021-09-11
The nuclear repressor BACH1 is known to control HO-1 expression together with the transcriptional activator NRF2. The results of our study show that HO-1 gene expression in LPS-stimulated macrophages is primarily regulated via BACH1. This idea is supported by a series of experimental evidence demons
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br Results and discussion br Conclusions A series
2021-09-11
Results and discussion Conclusions A series of novel HDAC inhibitors comprising the thioquinazolinone were designed and synthesized. These derivatives were evaluated for their antiproliferative activities against several human cancer cell lines. Then we chose compounds 7a, 4i, 4o, and 4p to fu
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br STAR Methods br Acknowledgments We
2021-09-11
STAR★Methods Acknowledgments We thank Prof. Y. Tomari at the University of Tokyo for experimental advice and K. Hanada for technical assistance. This research was supported by Grants-in-Aid for Scientific Research on Innovative Areas “Nascent Chain Biology” (JP15H01548 and JP17H05677 to T.I. a
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br Acknowledgement br Introduction Malignant melanoma is an
2021-09-11
Acknowledgement Introduction Malignant melanoma is an aggressive and highly metastatic cancer. The incidence of malignant melanoma is increasing all over the world, and the population of patients with advanced melanoma is growing [1], [2]. Malignant melanoma is often resistant to conventional
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Through the analysis of various
2021-09-11
Through the analysis of various synthetic GPR40 agonists as reported in literature, we found that a number of these compounds contained a phenylpropanoic ck1 inhibitor motif which was inspired from naturally occurring medium to long chain fatty acids. For instance, in the early period of discovering
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The development of immobilization techniques
2021-09-11
The development of immobilization techniques for β-glucosidase offers a potential way to enable its reuse several times [13]. The aim of immobilization is to trap the enzyme within or on the surface of an insoluble material with retention of its catalytic activity [14]. The immobilization strategy a
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In conclusion our results show that multiple receptor popula
2021-09-10
In conclusion, our results show that multiple receptor populations can be expressed when α4, β3 and δ mRNAs are injected into Xenopus oocytes and include β3 homomeric; α4β3; and β3δ receptors. The previously unidentified β3δ can be differentiated pharmacologically from either β3, α4β3 and α4β3δ rece
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